期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 11, 期 22, 页码 3664-3673出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3ob40263k
关键词
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资金
- CNRS
- ANR [ANR-10-LABX-33, ANR-09-BLAN-0071]
- Paris Sud University
- Agence Nationale de la Recherche (ANR) [ANR-09-BLAN-0071] Funding Source: Agence Nationale de la Recherche (ANR)
The synthesis of 2-alpha-styrylpyridines has been carried out by using the coupling of polyoxygenated N-tosylhydrazones with various 2-halopyridines. We demonstrated that the use of a catalytic amount of PdCl2(MeCN)(2) in combination with a bidentate ferrocene DPPF or a monodentate alkyl phosphine (Bu2MeP)-Bu-t-HBF4 constitutes an efficient protocol for this coupling, providing 2-alpha-styrylpyridines 2 in satisfactory to good yields. Among several polyoxygenated derivatives 2 evaluated, compound 2aa was found to exhibit excellent antiproliferative and antimitotic activities comparable to that of the reference compound isoCA-4.
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